1. Field of the Invention
The present invention relates to a pharmaceutical dosage form which contains hyoscyamine and/or a pharmaceutically acceptable salt thereof in at least two different formulations with different release profiles. The present invention also relates to a process for manufacturing the dosage form and to methods for alleviating or treating conditions which can be alleviated by hyoscyamine.
2. Discussion of Background Information
Hyoscyamine has actions similar to atropine but is more potent in both its central and peripheral effects. It inhibits gastrointestinal propulsive motility and decreases gastric acid secretions. It also controls excessive pharyngeal, tracheal, and bronchial secretions. Physicians rely on its ability to relieve intestinal hypermotility by prescribing hyoscyamine, usually in the form of hyoscyamine sulfate, for the relief of diarrhea and accompanying intestinal and stomach cramping. It is also used by physicians in the treatment of diverticulitis. By reducing acid secretions in the stomach, hyoscyamine is also useful in the treatment of gastric ulcers. It can also be used to relieve visceral spasm and hypermotility in cystitis pylorospasm and associated abdominal cramps. In combination with appropriate analgesics, hyoscyamine is also used for relief of biliary and renal colic and as a drying agent in the relief of symptoms of acute rhinitis. Hyoscyamine is also used in the treatment of irritable bowel syndrome, urinary incontinence and acute enterocolitis and related gastrointestinal disorders. Hyoscyamine further is indicated for the amelioration of allergic reactions, the treatment of motion sickness and the prevention and control of nausea and vomiting associated with certain types of anesthesia and surgery.
Once absorbed, hyoscyamine disappears rapidly from the blood and maintains therapeutic levels for approximately 3.5 hours. The majority of hyoscyamine is excreted in the urine unchanged within the first 12 hours.
Patients suffering from excessive gastrointestinal propulsive motility, excessive gastric acid secretions, excessive pharyngeal, tracheal, and bronchial secretions and symptoms of intestinal hypermotility such as diarrhea, intestinal and stomach cramping, diverticulitis, gastric ulcers, visceral spasm, cystitis pylorospasm, biliary and renal colic, irritable bowel syndrome, urinary incontinence, acute enterocolitis and related gastrointestinal disorders as well as patients suffering from acute rhinitis and related allergic symptoms and patients suffering motion sickness and nausea and vomiting may endure periods of 6 hours per day without adequate control of their symptoms if they are prescribed conventional hyoscyamine sulfate tablets or liquids. Dosages of these products are prescribed at intervals of 4 hours. With such dosages, the therapeutic level of the product is reached in about 30 minutes to one hour after ingestion and falls below therapeutic levels 30 minutes to over an hour before the next dose is taken. Even if patients ingest sustained-release or timed-release tablets, they must endure as many as 4 hours per day without adequate control of their symptoms, due to the slow release of the timed-release or sustained release product from the matrix in which hyoscyamine sulfate is embedded.